In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study

Several in vitro and in vivo studies have shown antidiabetic potential of flavonoids. These polyphenolic compounds biochemical properties are in fact structure dependent, however, yet to be clearly understood. Hence, the chief objective of this study was to determine the antidiabetic activities of s...

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Main Authors: Sarian, Murni Nazira, Ahmed, Qamar Uddin, Alhassan, Alhassan Muhammad, Bakhtiar, M. Taher, Arief Ichwan, Solachuddin Jauhari, Latip, Jalifah
Format: Conference or Workshop Item
Language:English
Published: 2018
Subjects:
Online Access:http://irep.iium.edu.my/63542/
http://irep.iium.edu.my/63542/1/63542_In%20vitro%20antidiabetic%20effects%20of%20flavonoids.pdf
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recordtype eprints
spelling iium-635422018-06-26T04:22:18Z http://irep.iium.edu.my/63542/ In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study Sarian, Murni Nazira Ahmed, Qamar Uddin Alhassan, Alhassan Muhammad Bakhtiar, M. Taher Arief Ichwan, Solachuddin Jauhari Latip, Jalifah QD Chemistry Several in vitro and in vivo studies have shown antidiabetic potential of flavonoids. These polyphenolic compounds biochemical properties are in fact structure dependent, however, yet to be clearly understood. Hence, the chief objective of this study was to determine the antidiabetic activities of some structurally related flavonoids to recognize important positions responsible, their correlation, as well as the effect of derivatisation on the same properties. 15 selected flavonoids were subjected to cytotoxicity test (MTT) on two different cell lines namely RIN-5F pancreatic and 3T3-L1 pre-adipocytes. Subsequently, the compounds were subjected to in vitro antidiabetic investigation using RIN-5F to determine the insulin secretagogue activity via ELISA as well as on 3T3-L1 adipocytes to determine the insulin sensitizing activity via adipogenesis and fluorescence glucose uptake tests. Next, the adipokines viz. leptin, tumor necrosis factor-α (TNF-α), adiponectin, and retinol binding protein-4 (RBP-4) were measured to investigate the biochemical reactions. Afterward, western blotting was performed to check GLUT4, PPARγ and PPARα protein expressions. To further understand the mechanism, molecular docking study was executed against same proteins. The structures of all flavonoids were elucidated through 1H-and 13C-NMR spectroscopy. Results showed that the total number and the configuration of hydroxyl groups, presence of C-2-C-3 double bond as well as C-4 ketonic group play important roles in regulating antidiabetic activity which help to enhance the glucose uptake via PPAR and GLUT4 protein receptors. The results might prove worthy of developing semi-synthetic analogs that may retain substantial antidiabetic capacity. 2018-03-19 Conference or Workshop Item NonPeerReviewed application/pdf en http://irep.iium.edu.my/63542/1/63542_In%20vitro%20antidiabetic%20effects%20of%20flavonoids.pdf Sarian, Murni Nazira and Ahmed, Qamar Uddin and Alhassan, Alhassan Muhammad and Bakhtiar, M. Taher and Arief Ichwan, Solachuddin Jauhari and Latip, Jalifah (2018) In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study. In: 34th International Conference on Natural Products 2018 (ICNP 2018), 19th-21st March 2018, Penang, Malaysia.
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
topic QD Chemistry
spellingShingle QD Chemistry
Sarian, Murni Nazira
Ahmed, Qamar Uddin
Alhassan, Alhassan Muhammad
Bakhtiar, M. Taher
Arief Ichwan, Solachuddin Jauhari
Latip, Jalifah
In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
description Several in vitro and in vivo studies have shown antidiabetic potential of flavonoids. These polyphenolic compounds biochemical properties are in fact structure dependent, however, yet to be clearly understood. Hence, the chief objective of this study was to determine the antidiabetic activities of some structurally related flavonoids to recognize important positions responsible, their correlation, as well as the effect of derivatisation on the same properties. 15 selected flavonoids were subjected to cytotoxicity test (MTT) on two different cell lines namely RIN-5F pancreatic and 3T3-L1 pre-adipocytes. Subsequently, the compounds were subjected to in vitro antidiabetic investigation using RIN-5F to determine the insulin secretagogue activity via ELISA as well as on 3T3-L1 adipocytes to determine the insulin sensitizing activity via adipogenesis and fluorescence glucose uptake tests. Next, the adipokines viz. leptin, tumor necrosis factor-α (TNF-α), adiponectin, and retinol binding protein-4 (RBP-4) were measured to investigate the biochemical reactions. Afterward, western blotting was performed to check GLUT4, PPARγ and PPARα protein expressions. To further understand the mechanism, molecular docking study was executed against same proteins. The structures of all flavonoids were elucidated through 1H-and 13C-NMR spectroscopy. Results showed that the total number and the configuration of hydroxyl groups, presence of C-2-C-3 double bond as well as C-4 ketonic group play important roles in regulating antidiabetic activity which help to enhance the glucose uptake via PPAR and GLUT4 protein receptors. The results might prove worthy of developing semi-synthetic analogs that may retain substantial antidiabetic capacity.
format Conference or Workshop Item
author Sarian, Murni Nazira
Ahmed, Qamar Uddin
Alhassan, Alhassan Muhammad
Bakhtiar, M. Taher
Arief Ichwan, Solachuddin Jauhari
Latip, Jalifah
author_facet Sarian, Murni Nazira
Ahmed, Qamar Uddin
Alhassan, Alhassan Muhammad
Bakhtiar, M. Taher
Arief Ichwan, Solachuddin Jauhari
Latip, Jalifah
author_sort Sarian, Murni Nazira
title In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
title_short In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
title_full In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
title_fullStr In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
title_full_unstemmed In vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
title_sort in vitro antidiabetic effects of flavonoids: molecular and structure-activity relationship based study
publishDate 2018
url http://irep.iium.edu.my/63542/
http://irep.iium.edu.my/63542/1/63542_In%20vitro%20antidiabetic%20effects%20of%20flavonoids.pdf
first_indexed 2018-09-07T08:14:08Z
last_indexed 2018-09-07T08:14:08Z
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